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33 results on '"Rigdon, Greg C"'

7. In Vivo Profile of ICA-27243 [N-(6-Chloro-pyridin-3-yl)-3,4-difluoro-benzamide], a Potent and Selective KCNQ2/Q3 (Kv7.2/Kv7.3) Activator in Rodent Anticonvulsant Models

Author

Roeloffs, Rosemarie, primary, Wickenden, Alan D., additional, Crean, Christopher, additional, Werness, Stephen, additional, McNaughton-Smith, Grant, additional, Stables, James, additional, McNamara, James O., additional, Ghodadra, Neil, additional, and Rigdon, Greg C., additional

Published
2008
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10. Indanylidenes. 1. Design and Synthesis of (E)-2-(4,6-Difluoro-1-indanylidene)acetamide, a Potent, Centrally Acting Muscle Relaxant with Antiinflammatory and Analgesic Activity

Author

Musso, David L., primary, Cochran, Felicia R., additional, Kelley, James L., additional, McLean, Ed W., additional, Selph, Jeffrey L., additional, Rigdon, Greg C., additional, Orr, G. Faye, additional, Davis, Ronda G., additional, Cooper, Barrett R., additional, Styles, Virgil L., additional, Thompson, James B., additional, and Hall, William R., additional

Published
2002
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23. Role of the nucleus basalis in conditioned responses of cortical neurons in the rat

Author

Rigdon, Greg C

Subjects
Rats -- Physiology, Neurons, Frontal lobes, Conditioned response, Acetylcholine -- Receptors
Abstract

Neurons in the rat frontal cortex demonstrate altered firing rates in response to conditioned stimuli. Experiments were designed to test the hypothesis that the basal forebrain cholinergic systera is involved in the generation of conditioned neuronal responses in the rat frontal cortex. Most of the cholinergic innervation to the frontal cortex is supplied by projections frora the nucleus basalis raagnocellularis (nBM), A two-second tone cue imraediately followed by rewarding medial forebrain bundle stimulation was used to elicit the conditioned neuronal responses in the following experiraents. Experiment One was performed to determine the effects of inhibiting the firing of neurons in the nBM region on the conditioned responses. This was presuraably accomplished by microinjecting procaine, a local anesthetic, or GABA, an inhibitory neurotransraitter, into the nBM region. Procaine antagonized the conditioned responses of 86% of the cortical single units tested and GABA antagonized the responses of 81% of the units. Experiment Two was designed to investigate the effects of blocking cholinergic receptors on the conditioned responses of frontal cortex neurons. Microinjection of atropine, a cholinergic antagonist, into the frontal cortex suppressed the conditioned responses of 21 of 24 cortical single units. The nBM region was lesioned with kainic acid, a neurotoxin, in Experiment Three. The lesion resulted in a significant decrease in choline acetyltransferase activity in the frontal cortex ipsilateral to the nBM lesion. Only 25% of the neurons recorded in the frontal cortex on the side of the nBM lesion exhibited conditioned responses. This was significantly lower than the percentage of neurons that exhibited conditioned responses (70%) in the cortex of untreated animals. The firing rates of units in the nBM region were monitored during the cue-event paradigm in Experiment Four. Of the 38 unit recordings from the nBM region, 28 (74%) exhibited conditioned responses. The results from the four experiments together provide strong evidence for a role of the basal forebrain cholinergic system in the generation of conditioned single unit responses in the frontal cortex.

Published
1985

32. Indanylidenes. 1. Design and synthesis of (E)-2-(4,6-difluoro-1-indanylidene)acetamide, a potent, centrally acting muscle relaxant with antiinflammatory and analgesic activity.

Author

Musso DL, Cochran FR, Kelley JL, McLean EW, Selph JL, Rigdon GC, Orr GF, Davis RG, Cooper BR, Styles VL, Thompson JB, and Hall WR

Subjects
Acetamides chemistry, Acetamides pharmacology, Analgesics chemistry, Analgesics pharmacology, Animals, Anti-Inflammatory Agents, Non-Steroidal chemistry, Anti-Inflammatory Agents, Non-Steroidal pharmacology, Hypnotics and Sedatives chemical synthesis, Hypnotics and Sedatives chemistry, Hypnotics and Sedatives pharmacology, Indans chemistry, Indans pharmacology, Mice, Monoamine Oxidase metabolism, Monoamine Oxidase Inhibitors chemical synthesis, Monoamine Oxidase Inhibitors chemistry, Monoamine Oxidase Inhibitors pharmacology, Muscle Relaxants, Central chemistry, Muscle Relaxants, Central pharmacology, Rats, Rats, Inbred Lew, Rats, Wistar, Stereoisomerism, Structure-Activity Relationship, Acetamides chemical synthesis, Analgesics chemical synthesis, Anti-Inflammatory Agents, Non-Steroidal chemical synthesis, Indans chemical synthesis, Muscle Relaxants, Central chemical synthesis
Abstract

The design of rigid cyclic analogues derived from cinnamamide 1, (E)-N-cyclopropyl-3-(3-fluorophenyl)prop-2-enamide, and beta-methylcinnamamide 2, (E)-N-cyclopropyl-3-(3-fluorophenyl)but-2-enamide, has led to the discovery of the potent, centrally acting muscle relaxant (E)-2-(4,6-difluoro-1-indanylidene)acetamide, 17. Compound 17 also possesses potent antiinflammatory and analgesic activity. This paper describes the synthesis and the muscle relaxant, antiinflammatory, and analgesic structure-activity relationships of 17 and 67 of its analogues. Compound 17 has been taken into phase I clinical trials.

Published
2003
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33. Indanylidenes. 2. Design and synthesis of (E)-2-(4-chloro-6-fluoro-1-indanylidene)-N-methylacetamide, a potent antiinflammatory and analgesic agent without centrally acting muscle relaxant activity.

Author

Musso DL, Orr GF, Cochran FR, Kelley JL, Selph JL, Rigdon GC, Cooper BR, and Jones ML

Subjects
Acetamides chemistry, Acetamides pharmacology, Analgesics chemistry, Analgesics pharmacology, Animals, Anti-Inflammatory Agents, Non-Steroidal chemistry, Anti-Inflammatory Agents, Non-Steroidal pharmacology, Hypnotics and Sedatives chemical synthesis, Hypnotics and Sedatives chemistry, Hypnotics and Sedatives pharmacology, Indans chemistry, Indans pharmacology, Mice, Muscle Relaxants, Central chemical synthesis, Muscle Relaxants, Central chemistry, Muscle Relaxants, Central pharmacology, Rats, Stereoisomerism, Structure-Activity Relationship, Acetamides chemical synthesis, Analgesics chemical synthesis, Anti-Inflammatory Agents, Non-Steroidal chemical synthesis, Indans chemical synthesis
Abstract

Extension of the structure-activity relationship studies that led to the discovery of the nonsedating potent muscle relaxant, antiinflammatory, and analgesic agent (E)-2-(4,6-difluoro-1-indanylidene)acetamide, 1, has given rise to (E)-2-(4-chloro-6-fluoro-1-indanylidene)-N-methylacetamide, 2. Compound 2 is a potent antiinflammatory and analgesic agent without centrally acting muscle relaxant activity.

Published
2003
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